Courtens Charlotte, Risseeuw Martijn, Caljon Guy, Cos Paul, Van Calenbergh Serge
Laboratory for Medicinal Chemistry, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
Laboratory for Microbiology, Parasitology and Hygiene, University of Antwerp, Universiteitsplein 1 (S7), B-2610 Wilrijk, Belgium.
ACS Med Chem Lett. 2018 Sep 11;9(10):986-989. doi: 10.1021/acsmedchemlett.8b00223. eCollection 2018 Oct 11.
Two classes of prodrugs of a fosmidomycin surrogate were synthesized and investigated for their ability to inhibit growth of and . To this end, a novel efficient synthesis route was developed involving a cross metathesis reaction as a key step. Alkoxyalkyl prodrugs show decent antimalarial activities, but acyloxybenzyl prodrugs proved to be the most interesting and show enhanced antimalarial and antitubercular activity. The most active antimalarial analogues show low nanomolar IC values.
合成了两类磷霉素替代物的前药，并研究了它们抑制[具体对象1]和[具体对象2]生长的能力。为此，开发了一种新颖高效的合成路线，其中交叉复分解反应是关键步骤。烷氧基烷基前药显示出良好的抗疟活性，但酰氧基苄基前药被证明是最具吸引力的，且显示出增强的抗疟和抗结核活性。最具活性的抗疟类似物显示出低纳摩尔的半数抑制浓度（IC）值。
